Alteration of the phosphorylation state of p34cdc2 kinase by the flavone L86-8275 in breast carcinoma cells. Correlation with decreased H1 kinase activity.

abstract：:Phomopsins comprise a family of peptide mycotoxins containing a 13-membered ring formed by an ether bridge, produced by the fungus Phomopsis leptostromiformis, the causal agent in lupin poisoning (lupinosis). The biochemical actions of two naturally occurring phomopsins, phomopsin A and B, and the chemical derivatives...

journal_title：Biochemical pharmacology

authors： Lacey E,Edgar JA,Culvenor CC

更新日期：1987-07-01 00:00:00

abstract：:It has been reported that endothelins (ETs) stimulate catecholamine release from chromaffin cells. However, it is not known whether ETs also affect catecholamine biosynthesis. Thus, using a rat pheochromocytoma cell line, PC12, we examined the effects of ETs on catecholamine biosynthesis. The mRNA level and activity o...

journal_title：Biochemical pharmacology

authors： Takekoshi K,Ishii K,Shibuya S,Kawakami Y,Isobe K,Nakai T

更新日期：2002-03-01 00:00:00

abstract：:The role of Ca2+ and protein kinase C (PKC) activity in the release of immunoreactive endothelin-1 (ET-1) from cultured porcine aortic endothelial cells of first or second passage has been studied. ET-1 accumulation within cells and secretion into cell-conditioned medium over 3 and/or 5 hr was measured. Confluent cell...

journal_title：Biochemical pharmacology

authors： Brunner F

更新日期：1995-06-16 00:00:00

abstract：:The murine Cyp2a-4 and Cyp2a-5 genes encode P450 isoforms catalysing testosterone 15 alpha-hydroxylase and coumarin 7-hydroxylase (COH) activities, respectively. Two days after the administration of a hepatotoxic dose of cerium chloride (2 mg/kg i.v.), COH activity was increased 3.2-fold in the liver of DBA/2 mice. Th...

journal_title：Biochemical pharmacology

authors： Salonpää P,Iscan M,Pasanen M,Arvela P,Pelkonen O,Raunio H

更新日期：1992-10-06 00:00:00

abstract：:An Ehrlich ascites tumour cell line (EHR2) was selected for resistance to etoposide (VP16) by in vivo exposure to this agent. The resulting cell line (EHR2/VP16) was 114.3-, 5.7-, and 4.0-fold resistant to VP16, daunorubicin, and vincristine, respectively. The amount of salt-extractable immunoreactive topoisomerase II...

journal_title：Biochemical pharmacology

authors： Nielsen D,Maare C,Eriksen J,Litman T,Friche E,Skovsgaard T

更新日期：2000-08-01 00:00:00

abstract：:The discipline of biochemical pharmacology emerged in the late 1940s as a result of an increasing emphasis on understanding drug mechanisms at the cellular level. This research approach has contributed significantly to the development of many new drug classes including antihypertensive, antifective, cholesterol loweri...

journal_title：Biochemical pharmacology

authors： Enna SJ,Feuerstein GZ,Piette J,Williams M

更新日期：2008-07-01 00:00:00

abstract：:Antibody-directed enzyme prodrug therapy (ADEPT) aims at the specific activation of a prodrug by an enzyme-immunoconjugate localized in tumor tissue. The use of an enzyme of human origin is preferable in ADEPT because it might not be immunogenic when administered to patients. In the case of human beta-glucuronidase, p...

journal_title：Biochemical pharmacology

authors： Houba PH,Leenders RG,Boven E,Scheeren JW,Pinedo HM,Haisma HJ

更新日期：1996-08-09 00:00:00

abstract：:Enhanced oxidative stress has been suggested to be involved in the degeneration of nigrostriatal dopaminergic neurons in Parkinson's disease. The high turnover rate of dopamine and/or unsequestered dopamine may cause an increase of formation of hydrogen peroxide via either oxidative deamination of dopamine by monoamin...

journal_title：Biochemical pharmacology

authors： Lai CT,Yu PH

更新日期：1997-02-07 00:00:00

abstract：:The multidrug resistance (MDR) phenotype is the major cause of failure of cancer chemotherapy. This phenotype is mainly due to the overexpression of the human MDR1 (hMDR1) gene. Several studies have shown that transcriptional regulation of this gene is unexpectedly complex and is far from being completely understood. ...

journal_title：Biochemical pharmacology

authors： Labialle S,Gayet L,Marthinet E,Rigal D,Baggetto LG

更新日期：2002-09-01 00:00:00

abstract：:Wild-type and repair-deficient cell lines ( EM9 ) of Chinese Hamster Ovary cells were utilized to assess cytotoxic responses towards metals that produce lesions in DNA. Alkaline elution studies indicated that both CaCrO4 and HgCl2 induced single-strand breaks in the DNA. CaCrO4 and HgCl2 treatments of intact Chinese h...

journal_title：Biochemical pharmacology

authors： Christie NT,Cantoni O,Evans RM,Meyn RE,Costa M

更新日期：1984-05-15 00:00:00

abstract：:N,N-Dimethyl-D-erythro-sphingosine (DMS) is the N-methyl derivative of sphingosine; both are activators of sphingosine-dependent protein kinases. The aim of this work was to study the effect of DMS on cytosolic calcium and intracellular pH (pHi) in human T lymphocytes. The variations of calcium and pH were determined ...

journal_title：Biochemical pharmacology

authors： Alfonso A,De la Rosa LA,Vieytes MR,Botana LM

更新日期：2003-02-01 00:00:00

abstract：:Overactive bladder (OAB) syndrome is a prevalent condition of the lower urinary tract that causes symptoms, such as urinary frequency, urinary urgency, urge incontinence, and nocturia, and disproportionately affects women and the elderly. Current medications for OAB merely provide symptomatic relief with considerable ...

journal_title：Biochemical pharmacology

authors： Hou R,Yu Y,Jiang J

更新日期：2020-12-09 00:00:00

abstract：:Histone deacetylases (HDAC) play a key role in regulating gene expression by deacetylating histones. Some HDAC isoforms can also modulate the function of nonhistone proteins implicated in regulatory processes, and therefore HDACs are recognized as useful targets for therapeutic purposes. HDAC inhibitors have generated...

journal_title：Biochemical pharmacology

authors： Dallavalle S,Pisano C,Zunino F

更新日期：2012-09-15 00:00:00

abstract：:In assessing the biological effects of exposure to a complex chemical mixture, it is important to determine how the behavior of one compound may be influenced by the presence of other compounds in the mixture. In this study the effect of pre-exposure to an organic extract of diesel exhaust or to selected compounds in ...

journal_title：Biochemical pharmacology

authors： Howard AJ,Mitchell CE,Dutcher JS,Henderson TR,McClellan RO

更新日期：1986-07-01 00:00:00

abstract：:The over-expression of ABCC1 transmembrane protein has been shown to cause multidrug resistance in tumor cell lines. ABCC1 is a member of the ABC transmembrane proteins that function as efflux pumps with diverse substrate specificity. Several endogenous cell metabolites, including the leukotriene C4 (LTC(4)) and gluta...

journal_title：Biochemical pharmacology

authors： Laberge RM,Karwatsky J,Lincoln MC,Leimanis ML,Georges E

更新日期：2007-06-01 00:00:00

abstract：:Eg5, the product of Kif11 gene, also known as kinesin spindle protein, is a motor protein involved in the proper establishment of a bipolar mitotic spindle. Eg5 is one of the 45 different kinesins coded in the human genome of the kinesin motor protein superfamily. Over the last three decades Eg5 has attracted great in...

journal_title：Biochemical pharmacology

authors： Garcia-Saez I,Skoufias DA

更新日期：2020-12-11 00:00:00

abstract：:Indole alkaloids possess a large spectrum of biological activities including anti-protozoal action. Here we report for the first time that voacamine, isolated from the plant Tabernaemontana coronaria, is an antiprotozoal agent effective against a large array of trypanosomatid parasites including Indian strain of Leish...

journal_title：Biochemical pharmacology

authors： Chowdhury SR,Kumar A,Godinho JLP,De Macedo Silva ST,Zuma AA,Saha S,Kumari N,Rodrigues JCF,Sundar S,Dujardin JC,Roy S,De Souza W,Mukhopadhyay S,Majumder HK

更新日期：2017-08-15 00:00:00

abstract：:Stimulation of human gingival fibroblasts with histamine elicited an increase in the intracellular concentration of free calcium ([Ca2+]i) and the formation of inositol 1,4,5-trisphosphate (InsP3) in a concentration- and time-dependent manner. The histamine-induced increase in [Ca2+]i was attenuated completely by chlo...

journal_title：Biochemical pharmacology

authors： Niisato N,Ogata Y,Furuyama S,Sugiya H

更新日期：1996-10-11 00:00:00

abstract：:Incubation of rat peritoneal mast cells with hydrogen peroxide results in a marked release of histamine. Maximal release is observed with 0.05-0.1 mM H(2)O(2), but higher concentrations of H(2)O(2) instead suppresses the release. Histamine release starts after about 2 min of lag time and reaches a plateau in about 10 ...

journal_title：Biochemical pharmacology

authors： Ohmori H,Yamamoto I,Akagi M,Tasaka K

更新日期：1980-03-01 00:00:00

abstract：:A compound, YM-53792, was identified as an inhibitor of interleukin-2 (IL-2) gene promoter activity, using a Jurkat cell-based reporter system in which the luciferase gene is regulated by the IL-2 gene promoter. Production of IL-2, interleukin-4 (IL-4) and interleukin-5 (IL-5) from human peripheral blood mononuclear c...

journal_title：Biochemical pharmacology

authors： Kuromitsu S,Fukunaga M,Lennard AC,Masuho Y,Nakada S

更新日期：1997-11-01 00:00:00

abstract：:The crude mitochondrial fraction of rat brain contains an active dehydrogenase involved in the direct oxidation of gamma-aminobutyric acid. INT (p-iodonitrotetrazolium violet) can serve as an efficient acceptor of electrons in this dehydrogenase reaction. During this oxidation of GABA, ammonia is not produced. In vitr...

journal_title：Biochemical pharmacology

authors： Banerjee A,Turner AJ,Guha SR

更新日期：1982-10-15 00:00:00

abstract：:The effect of 2-(2,5-dimethoxyphenylmethyl)-3-(2-dimethylaminoethyl)- 6-isopropoxy-4(3H)-quinazolinone hydrochloride (MCI-176), a calcium antagonist, on ischemic myocardial metabolism was studied in dog hearts subjected to an occlusion of the left anterior descending coronary artery (LAD) for 3 or 30 min. MCI-176 (0.0...

journal_title：Biochemical pharmacology

authors： Abe Y,Ichihara K,Abiko Y

更新日期：1991-02-01 00:00:00

abstract：:GABAB receptors assemble from GABAB1 and GABAB2 subunits. GABAB2 additionally associates with auxiliary KCTD subunits (named after their K(+) channel tetramerization-domain). GABAB receptors couple to heterotrimeric G-proteins and activate inwardly-rectifying K(+) channels through the βγ subunits released from the G-p...

journal_title：Biochemical pharmacology

authors： Adelfinger L,Turecek R,Ivankova K,Jensen AA,Moss SJ,Gassmann M,Bettler B

更新日期：2014-10-01 00:00:00

abstract：:5-Phenylthioacyclouridine (PTAU or 1-[(2-hydroxyethoxy)methyl]-5-phenylthiouracil) was synthesized as a highly specific and potent inhibitor of uridine phosphorylase (UrdPase, EC 2.4.2.3). PTAU has inhibition constant (K(is)) values of 248 and 353 nM towards UrdPase from mouse and human livers, respectively. PTAU was ...

journal_title：Biochemical pharmacology

authors： el Kouni MH,Goudgaon NM,Rafeeq M,Al Safarjalani ON,Schinazi RF,Naguib FN

更新日期：2000-09-15 00:00:00

abstract：:Naturally soluble rat germ cell adenylate cyclase was inhibited by adenosine and the adenosine analogs, 9-beta-D-arabinofuranosyl adenine (AFA) and 2',5'-dideoxyadenosine (DDA), all of which inhibited hormone-sensitive adenylate cyclases at the "P" site. The IC50 values for adenosine and DDA were approximately 0.1 and...

journal_title：Biochemical pharmacology

authors： Onoda JM,Braun T,Wrenn SM Jr

更新日期：1987-06-15 00:00:00

abstract：:Aldehydes generated during radical-induced lipid peroxidation, in particular 4-hydroxynonenal, are known to inhibit growth of certain cells. To extend our arguments that free radicals might be involved in the host response against malaria parasites we tested 26 carbonyls (n-alkanals, C6-C11; 2-alkenals, C3-C9; 2,4-alk...

journal_title：Biochemical pharmacology

authors： Clark IA,Butcher GA,Buffinton GD,Hunt NH,Cowden WB

更新日期：1987-02-15 00:00:00

abstract：:Pancreatic stellate cells (PSCs) play a key role in pancreatic fibrosis, a constant feature of chronic pancreatitis. PSC activation occurs in response to profibrogenic mediators such as cytokines and involves proliferation, transition towards a myofibroblastic phenotype and enhanced production of extracellular matrix ...

journal_title：Biochemical pharmacology

authors： Jaster R,Brock P,Sparmann G,Emmrich J,Liebe S

更新日期：2003-04-15 00:00:00

abstract：:Human chronic myelogenous leukemia (CML) cell line K562 can be chemically induced to differentiate and express embryonic and fetal globin genes. In this study, the effects of doxorubicin (DOX), an inducer of K562 cell erythroid differentiation, with those of epidoxorubicin (EDOX) as well as newly synthesized derivativ...

journal_title：Biochemical pharmacology

authors： Szulawska A,Arkusinska J,Czyz M

更新日期：2007-01-15 00:00:00

abstract：:We examined the effects of the divalent cation calcium (Ca2+) and the monovalent cations potassium (K+) and sodium (Na+) and different modalities that affect the fluxes of these cations on immunoreactive secretin (IRS) secretion from canine duodenal mucosa in vitro. In the absence of extracellular Ca2+, the basal IRS ...

journal_title：Biochemical pharmacology

authors： Murthy SN,Lavy A

更新日期：1988-03-15 00:00:00

abstract：:The effect of oxidant stress produced by redox cycling of substituted 1,4-naphthoquinones on the activity of platelet (Na(+)-K+)ATPase and the active transport of serotonin (5-HT) was studied. 2-Methyl-1,4-naphthoquinone (menadione) produced a concentration-dependent (0-100 microM) and time-dependent (2-20 min) stimul...

journal_title：Biochemical pharmacology

authors： Bosin TR,Schaltenbrand SL

更新日期：1991-03-15 00:00:00